Uses and Common Adverse Effects of Cabergoline

Cabergoline is a dopamine D2 receptor agonist that is often prescribed for the treatment of hyperprolactinemia. This Buzzle write-up provides information on the uses and common side effects of cabergoline.
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Use of Cabergoline
Did You Know?
Though cabergoline was invented in the early '80s, it was approved by the FDA on December 23, 1996.
Marketed under the brand name Dostinex and Cabaser, cabergoline is an ergot-derived drug, which means that it is derived from a group of fungi from the genus Claviceps. Since late 2005, it is available as a generic medicine, which means, it is marketed without a brand name. It must be noted that generic drugs are chemically identical to drugs that are sold under brand names.

The active ingredient of both Dostinex, as well as Cabaser is cabergoline. However, Cabaser contains larger doses of cabergoline. Dostinex is mainly prescribed for medical conditions that are characterized by high levels of prolactin in the blood. Cabaser is prescribed for managing the symptoms of Parkinson's disease. It must be noted that Dostinex is not licensed for use in case of individuals affected by Parkinson's disease.

How Does Cabergoline Work

Cabergoline belongs to a class of drugs called dopamine receptor agonists. These are drugs that activate the dopamine receptors in the absence of dopamine. Dopamine is a monoamine neurotransmitter that is essential for the normal functioning of the central nervous system. It also acts as a prolactin-inhibiting factor, which means that it reduces the production of prolactin from the pituitary gland. Prolactin cells in the anterior pituitary gland synthesize prolactin in response to signals from dopamine and thyrotropin-releasing hormone, which exert inhibitory and secretagogue effects, respectively. Oxytocin, estrogen, and progesterone also regulate the secretion of prolactin. Since dopamine has an inhibitory effect on prolactin, low levels of dopamine are bound to give rise to hyperprolactinemia. Under such circumstances, dopamine receptor agonists are prescribed. Cabergoline is a long-acting dopamine receptor agonist that activates the D2 receptors that are found on the pituitary gland, which in turn reduces the amount of prolactin secreted by the pituitary gland.

Uses

Prolactin is a hormone that stimulates lactation after childbirth. Hyperprolactinemia could occur due to a prolactin-secreting tumor (prolactinoma), pregnancy, the use of certain medication, or the presence of a pituitary tumor that is putting pressure on the pituitary gland. Women affected by this condition are likely to experience irregularities or changes in the menstrual cycle, reduced sex drive, increased secretion of breast milk, and infertility. In case of premenopausal women, the contributing factor could be a tumor. Men who are affected by this condition could develop symptoms such as enlarged breasts, progressive loss of libido, low sperm count, decreased sexual ability, etc. Dostinex can help reduce the amount of prolactin, thereby reducing the aforementioned symptoms.

Besides the aforementioned condition, higher doses of cabergoline, which is marketed under the brand name Cabaser, are also prescribed for the treatment of Parkinson's disease (a neurological condition that is characterized by impairment of muscle coordination). Since dopamine helps the brain to control muscle movements, its deficiency can make one susceptible to this disease. Cabaser increases the effects of dopamine, which helps reduce the symptoms to some extent. However, caution must be exercised while using Cabaser. In two studies published in the New England Journal of Medicine in 2007, it was suggested that cabergoline and another drug named pergolide could cause valvular heart disease. While pergolide was taken off from the market, Cabaser is still available, as it has not been approved by the FDA for the treatment of Parkinson's disease.

Contraindications

Drug interactions could occur if the patient is taking medicines that belong to certain class of drugs such as butyrophenones, dopamine antagonists, ergot alkaloids, macrolides, medicines that lower blood pressure, phenothiazines, and thioxanthenes. Cabergoline might interact with erythromycin and metoclopramide. Thus, it is extremely essential to inform your doctor about the drugs that you are currently taking. Cabergoline should be taken as per the directions of the healthcare provider. It should not be taken by:

Those who are under 16 years of age
People who have liver problems
People who are allergic or sensitive to ergot alkaloids
People who have had an adverse reaction to ergot alkaloids in the past
Pregnant women (especially those affected by preeclampsia)
Nursing mothers
People affected by mental health problems
People affected by lung problems
People affected by peptic ulcers
People affected by gastrointestinal bleeding
People affected by heart or circulatory problems
People affected by Raynaud's syndrome
People affected by fibrosis or inflammation of an internal organ currently or in the past
People affected by low blood pressure

Adverse Effects

The side effects of this drug are fewer, in case it is being used for the treatment of hyperprolactinemia. The side effects might be related to the dosage, which is why side effects are more likely to be observed when it is taken in large doses. Some of the common side effects include:

Nausea
Vomiting
Stomach upset
Dry mouth
Constipation
Dizziness or lightheadedness while getting up too quickly from a lying position
Fatigue

Seek medical help, if you experience the following side effects:

Shortness of breath
Persistent cough
Swollen ankles or feet
Excessive fatigue
Behavioral or mood changes (nervousness, compulsive behavior)
Changes in the vision
Pain during menstruation
Pain in the breasts
Chest pain
Lower back/flank pain
Low blood pressure
Disturbed sleep or insomnia
Change in the amount of urine

Medical help must be immediately sought, if one develops an allergic reaction and experiences symptoms such as rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, difficulty breathing, etc.

The doses are in accordance with the patient's medical condition and the response to treatment. More often than not, a low dose is prescribed initially and increased gradually, depending on how the patient is responding. It is extremely essential to religiously follow the doctor's instructions regarding the dosage. One should always take it as per the prescribed dosage. If you miss a dose, take the missed dose as soon as you remember. Don't take a double dose, if it is almost time for the next dose. In case of any adverse effects, medical help must be sought immediately.

Disclaimer: The information provided in this article is solely for educating the reader. It is not intended to be a substitute for the advice of a medical expert.
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Published: June 30, 2014
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